3-Azatetracyclo[5.2.1.1(5,8).0(1,5)]undecane derivatives: from wild-type inhibitors of the M2 ion channel of influenza A virus to derivatives with potent activity against the V27A mutant.

@article{ReyCarrizo20133Azatetracyclo521158015undecane,
  title={3-Azatetracyclo[5.2.1.1(5,8).0(1,5)]undecane derivatives: from wild-type inhibitors of the M2 ion channel of influenza A virus to derivatives with potent activity against the V27A mutant.},
  author={Mat{\'i}as Rey-Carrizo and Eva Torres and Chunlong Ma and Marta Barniol-Xicota and Jun Wang and Yibing Wu and Lieve M J Naesens and William F. DeGrado and Robert A. Lamb and Lawrence H. Pinto and Santiago V{\'a}zquez},
  journal={Journal of medicinal chemistry},
  year={2013},
  volume={56 22},
  pages={9265-74}
}
We have synthesized and characterized a series of compounds containing the 3-azatetracyclo[5.2.1.1(5,8).0(1,5)]undecane scaffold designed as analogues of amantadine, an inhibitor of the M2 proton channel of influenza A virus. Inhibition of the wild-type (WT) M2 channel and the amantadine-resistant A/M2-S31N and A/M2-V27A mutant ion channels were measured in Xenopus oocytes using two-electrode voltage clamp (TEV) assays. Most of the novel compounds inhibited the WT ion channel in the low… CONTINUE READING
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